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    • 6. 发明公开
    • IMPROVED FLUORINATION PROCESS
    • 改进的氟化过程
    • EP3212597A1
    • 2017-09-06
    • EP15731300.8
    • 2015-06-22
    • Sandoz AG
    • SCHÖNE, OlgaWILHELM, ThorstenSPITZENSTÄTTER, Hans-PeterJUEN, Julia
    • C07B39/00C07H19/067C07H19/073
    • C07H19/06C07H1/00C07H19/10
    • A process comprising (i) providing a mixture comprising a compound of formula (I) or isomers, stereoisomers, diastereomers, enantiomers or salts thereof; (ii)subjecting the mixture provided in (i) to fluorinating conditions in the presence of a fluorination agent selected from the group consisting of diethylamino (difluoro) sulfonium tetrafluoroborate and difluoro(morpholino) sulfonium tetrafluoroborate obtaining a mixture comprising a compound of formula (II) or isomers, stereoisomers diastereomers, enantiomers or salts thereof; (iii) optionally subjecting the mixture obtained in (ii) to deprotection conditions, obtaining a mixture comprising the compound of formula (III) or isomers, stereoisomers, diastereomers, enantiomers or salts thereof.
    • (i)提供包含式(I)化合物或其异构体,立体异构体,非对映异构体,对映异构体或盐的混合物; (ii)使(i)中提供的混合物在选自二氟氨基(二氟)锍四氟硼酸盐和二氟(吗啉基)锍四氟硼酸盐的氟化剂存在下进行氟化条件,获得包含式(II) )或其异构体,立体异构体非对映异构体,对映异构体或盐; (iii)任选使(ii)中获得的混合物经历脱保护条件,获得包含式(III)化合物或其异构体,立体异构体,非对映异构体,对映异构体或盐的混合物。